Isoquinoline derivatives, pharmaceutical formulations based on these compounds and the use thereof

Abstract

Isoquinoline-4-carboxylic acid derivatives of the formula I ##STR1## in which m, n, R 1 , R 2 , R 3 , A and X have the meansings indicated, and physiologically acceptable acid addition salts thereof, a process for their preparation, pharmaceutical formulations based on these compounds and the use thereof as antiarrythmic agents.

We claim: 
     
       1. An isoquinoline-4-carboxylic acid derivative of the formula I ##STR18## in which m and n denote one or two, X denotes oxygen or nitrogen which is substituted by hydrogen or C 1  -C 6  -alkyl, A denotes a bond or a linear or branched C 1  -C 8  -alkylene chain,   R 1  either denotes an amino group of the formula ##STR19## in which R 4  and R 5  are identical or different and denote hydrogen or linear or branched C 1  -C 8  -alkyl radicals, or   R 1  denotes a 3-membered to 6-membered ring which has a nitrogen atom in the ring and in which the nitrogen atom is unsubstituted or substituted by hydrogen or C 1  -C 8  -alkyl and in which one --CH 2  -- group can be replaced by oxygen, sulfur or the --NH-- or --N--C 1  -C 8  -alkyl group, subject to the proviso that the hetero-atoms in the side chain (--X--A--R 1 ) are separated by at least 2 carbon atoms,   R 2  denotes hydrogen, fluorine, chlorine, bromine, hydroxyl, nitro, amino, C 1  -C 6  -alkyl or C 1  -C 6  -alkoxy radicals, and   R 3  denotes hydrogen, fluorine, chlorine, bromine, hydroxyl, nitro, amino, C 1  -C 6  -alkyl or C 1  -C 6  -alkoxy radicals or a benzyloxy, methylenedioxy or ethylenedioxy group,   or a physiologically acceptable acid addition salt thereof.   
     
     
       2. An isoquinoline-4-carboxylic acid derivative of the formula I indicated in claim 1, in which n is one, X is oxygen or nitrogen which is substituted by hydrogen, A is a linear C 2  to C 3  alkylene group, R 1  is an amino group of the formula ##STR20## in which R 4  and R 5  are identical and represent C 1  -C 3  -alkyl radicals, R 2  is hydrogen or C 1  -C 3  -alkyl and R 3  is hydrogen, or a physiologically acceptable acid addition salt thereof. 
     
     
       3. The compound N-(2-diethylamino)-ethyl)-1-(2-methylphenyl)-isoquinoline-4-carboxylyic acid amide or its hydrochloric acid salt. 
     
     
       4. A pharmaceutical formulation containing a pharmaceutically effective amount of a compound as claimed in claim 1. 
     
     
       5. A method of treating a host having arrythmias which comprises administering to said host a pharmaceutically effective dosage of a compound as claimed in claim 1. 
     
     
       6. The method as claimed in claim 5 wherein from 50 to 100 mg per day of said compound is injected intravenously into said host. 
     
     
       7. The method as claimed in claim 5 wherein from 100 to 300 mg per day of said compound is administered perorally to said host. 
     
     
       8. A method of treating a host having arrythmias which comprises administering to said host a pharmaceutically effective dosage of a compound as claimed in claim 3. 
     
     
       9. The method as claimed in claim 8 wherein from 50 to 100 mg per day of said compound is injected intravenously into said host. 
     
     
       10. The method as claimed in claim 8 wherein from 100 to 300 mg per day of said compound is administered perorally to said host.